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Design, synthesis and antitumor activity of novel 6,7-dimethoxyquinazoline derivatives containing diaryl urea moiety

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Chemical Research in Chinese Universities Aims and scope

Abstract

A series of 6,7-dimethoxyquinazoline derivatives connected by diaryl urea scaffolds was designed, synthesized and their in vitro antitumor activities were evaluated. Most of them showed an excellent potency against the four tested cancer cell lines as compared with sorafenib. Particularly, a promising compound 20 was identified, which showed the most potent antitumor activities with IC50 values of 0.08, 0.09, 0.16 and 0.19 µmol/L against H460, HT-29, MKN-45 and MDA-MB-231 cell lines, respectively. The structure-activity relationship(SAR) analysis indicated that compounds with dimethylamino or diethylamino group at the C4 position of 6,7-dimethoxyquinazoline moiety exhibited superior activities than compounds bearing morpholino groups.

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Authors and Affiliations

  1. Key Laboratory of Structure-based Drug Design and Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, P. R. China

    Yunlei Hou, Shasha Wu, Longsheng Ma, Jinying Bai, Zijian Liu & Yanfang Zhao

Authors
  1. Yunlei Hou
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  2. Shasha Wu
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  3. Longsheng Ma
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  4. Jinying Bai
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  5. Zijian Liu
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  6. Yanfang Zhao
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Corresponding author

Correspondence to Yanfang Zhao.

Additional information

Supported by the Program for Innovative Research Team of the Ministry of Education of the People’s Republic of China and Program for Liaoning Innovative Research Team in University, China(No.IRT1073) and the Liaoning Excellent Talents in University of China(No.LJQ2013106).

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Hou, Y., Wu, S., Ma, L. et al. Design, synthesis and antitumor activity of novel 6,7-dimethoxyquinazoline derivatives containing diaryl urea moiety. Chem. Res. Chin. Univ. 31, 766–773 (2015). https://doi.org/10.1007/s40242-015-5036-z

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  • DOI: https://doi.org/10.1007/s40242-015-5036-z

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